The reaction of P-diketones 1 with phenyl hydrazine afforded 5-aryl-3-(1- methyl-5-nitro-2-imidazoly1)-1-phenylpyrazole (2) and 3-aryl-5-(1-methyl-5- nitro-2-imidazoly1) -1-phenylpyrazole (3). The reaction of diketones (1) with urea in the presence of p-toluenesulfonic acid gave 4-(or 6-)aryl-6-(or 4-)(1-methyl- 5-nitro-2-imidazolyl)-1-(lH)pyrimidones (4). The structures of all compounds w...

Sodium selenate efficiently catalyzes the three-component Biginelli reaction of an aldehyde, a,βketo ester and urea or thiourea under solvent-free conditions to afford the corresponding 3,4-dihydropyrimidin2(1H)-ones or –thiones in excellent yields.

Lack of target specificity by existing matrix metalloproteinase (MMP) inhibitors has hindered antimetastatic cancer drug discovery. Inhibitors that bind to noncatalytic sites of MMPs and disrupt protease signaling function have the potential to be more specific and selective. In this work, compounds that target the hemopexin (PEX) domain of MMP-9 were identified using an in silico docking appro...

The parent barbituric acid and 2-thiobarbituric acid are convenient starting compounds for the preparation of different fused heterocycles and 5-substituted derivatives which are pharmacologically one of the most important classes of barbituric acid based compounds. The fused compounds of barbituric and thiobarbituric acid 7-(4-aminophenyl)-5-aryl5H-pyrano [2, 3-d] pyrimidinone, 5a-f have been ...

Bropirimine (ABPP), a pyrimidinone, is currently under clinical trial for its antitumor potential. Bropirimine alone was marginally active against some experimental tumors such as B16 melanoma but was ineffective against others such as P388 or L1210 leukemia. However, it produced statistically significant synergistic activity against P388 leukemia when used in combination with cyclophosphamide ...

Myristoylated alanine-rich C kinase substrate (MARCKS) protein has been recognized as a key regulatory molecule controlling mucin secretion by airway epithelial cells in vitro and in vivo. We recently showed that two intracellular chaperones, heat shock protein 70 (HSP70) and cysteine string protein (CSP), associate with MARCKS in the secretory mechanism. To elucidate more fully MARCKS-HSP70 in...

A new, efficient and mild approach for the oxidative dehydrogenation of dihydropyrimidinones and thiocyanation of aromatic compounds using 1,1,2,2-tetrahydroperoxy-1,2-diphenylethane (THPDPE) as a terminal oxidant was developed. Initially, various substrates bearing different electron-donating and electron-releasing functionalities were synthesized and next under the optimized reaction conditio...

Organic photovoltaics (OPVs) represent a potentially low-cost solution for harnessing solar energy and addressing global energy needs. 1 Organic photovoltaics can be broken down into two categories: polymer solar cells and small molecule solar cells. Polymer solar cells have so far achieved higher efficiencies because they typically exhibit superior device architecture compared to those of smal...